Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTXJIF13)

DOT Name Insulin-like growth factor 1 receptor (IGF1R)
Synonyms EC 2.7.10.1; Insulin-like growth factor I receptor; IGF-I receptor; CD antigen CD221
Gene Name IGF1R
Related Disease
Growth delay due to insulin-like growth factor I resistance ( )
UniProt ID
IGF1R_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
1IGR ; 1JQH ; 1K3A ; 1M7N ; 1P4O ; 2OJ9 ; 2ZM3 ; 3D94 ; 3F5P ; 3I81 ; 3LVP ; 3LW0 ; 3NW5 ; 3NW6 ; 3NW7 ; 3O23 ; 3QQU ; 4D2R ; 4XSS ; 5FXQ ; 5FXR ; 5FXS ; 5HZN ; 5U8Q ; 5U8R ; 6JK8 ; 6VWG ; 6VWH ; 6VWI ; 6VWJ ; 7PH8 ; 7S0Q ; 7S8V ; 7U23 ; 7V3P ; 7XGD ; 7XLC ; 7YRR ; 8PYI ; 8PYJ ; 8PYK ; 8PYL ; 8PYM ; 8PYN
EC Number
2.7.10.1
Pfam ID
PF00041 ; PF00757 ; PF07714 ; PF01030
Sequence
MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLH
ILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIF
EMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGD
LCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCS
APDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHD
GECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNL
LINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSF
YVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTR
NNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDG
QDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSE
ILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRH
NYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRK
VFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFES
RVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTW
EPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGN
YTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHR
KRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKG
VVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIME
LMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARN
CMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGV
VLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFL
EIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRH
SGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC
Function
Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involved in cell growth and survival control. IGF1R is crucial for tumor transformation and survival of malignant cell. Ligand binding activates the receptor kinase, leading to receptor autophosphorylation, and tyrosines phosphorylation of multiple substrates, that function as signaling adapter proteins including, the insulin-receptor substrates (IRS1/2), Shc and 14-3-3 proteins. Phosphorylation of IRSs proteins lead to the activation of two main signaling pathways: the PI3K-AKT/PKB pathway and the Ras-MAPK pathway. The result of activating the MAPK pathway is increased cellular proliferation, whereas activating the PI3K pathway inhibits apoptosis and stimulates protein synthesis. Phosphorylated IRS1 can activate the 85 kDa regulatory subunit of PI3K (PIK3R1), leading to activation of several downstream substrates, including protein AKT/PKB. AKT phosphorylation, in turn, enhances protein synthesis through mTOR activation and triggers the antiapoptotic effects of IGFIR through phosphorylation and inactivation of BAD. In parallel to PI3K-driven signaling, recruitment of Grb2/SOS by phosphorylated IRS1 or Shc leads to recruitment of Ras and activation of the ras-MAPK pathway. In addition to these two main signaling pathways IGF1R signals also through the Janus kinase/signal transducer and activator of transcription pathway (JAK/STAT). Phosphorylation of JAK proteins can lead to phosphorylation/activation of signal transducers and activators of transcription (STAT) proteins. In particular activation of STAT3, may be essential for the transforming activity of IGF1R. The JAK/STAT pathway activates gene transcription and may be responsible for the transforming activity. JNK kinases can also be activated by the IGF1R. IGF1 exerts inhibiting activities on JNK activation via phosphorylation and inhibition of MAP3K5/ASK1, which is able to directly associate with the IGF1R.; When present in a hybrid receptor with INSR, binds IGF1. PubMed:12138094 shows that hybrid receptors composed of IGF1R and INSR isoform Long are activated with a high affinity by IGF1, with low affinity by IGF2 and not significantly activated by insulin, and that hybrid receptors composed of IGF1R and INSR isoform Short are activated by IGF1, IGF2 and insulin. In contrast, PubMed:16831875 shows that hybrid receptors composed of IGF1R and INSR isoform Long and hybrid receptors composed of IGF1R and INSR isoform Short have similar binding characteristics, both bind IGF1 and have a low affinity for insulin.
Tissue Specificity
Found as a hybrid receptor with INSR in muscle, heart, kidney, adipose tissue, skeletal muscle, hepatoma, fibroblasts, spleen and placenta (at protein level). Expressed in a variety of tissues. Overexpressed in tumors, including melanomas, cancers of the colon, pancreas prostate and kidney.
KEGG Pathway
EGFR tyrosine ki.se inhibitor resistance (hsa01521 )
Endocrine resistance (hsa01522 )
MAPK sig.ling pathway (hsa04010 )
Ras sig.ling pathway (hsa04014 )
Rap1 sig.ling pathway (hsa04015 )
HIF-1 sig.ling pathway (hsa04066 )
FoxO sig.ling pathway (hsa04068 )
Oocyte meiosis (hsa04114 )
Autophagy - animal (hsa04140 )
Endocytosis (hsa04144 )
mTOR sig.ling pathway (hsa04150 )
PI3K-Akt sig.ling pathway (hsa04151 )
AMPK sig.ling pathway (hsa04152 )
Longevity regulating pathway (hsa04211 )
Longevity regulating pathway - multiple species (hsa04213 )
Focal adhesion (hsa04510 )
Adherens junction (hsa04520 )
Sig.ling pathways regulating pluripotency of stem cells (hsa04550 )
Long-term depression (hsa04730 )
Ovarian steroidogenesis (hsa04913 )
Progesterone-mediated oocyte maturation (hsa04914 )
Pathways in cancer (hsa05200 )
Transcriptio.l misregulation in cancer (hsa05202 )
Proteoglycans in cancer (hsa05205 )
Glioma (hsa05214 )
Prostate cancer (hsa05215 )
Melanoma (hsa05218 )
Breast cancer (hsa05224 )
Hepatocellular carcinoma (hsa05225 )
Reactome Pathway
IRS-related events triggered by IGF1R (R-HSA-2428928 )
SHC-related events triggered by IGF1R (R-HSA-2428933 )
Extra-nuclear estrogen signaling (R-HSA-9009391 )
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) (R-HSA-2404192 )

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Growth delay due to insulin-like growth factor I resistance DISWL710 Definitive Autosomal dominant [1]
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Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 5 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Niclosamide DMJAGXQ Approved Insulin-like growth factor 1 receptor (IGF1R) affects the response to substance of Niclosamide. [59]
Bortezomib DMNO38U Approved Insulin-like growth factor 1 receptor (IGF1R) increases the response to substance of Bortezomib. [60]
Etoposide DMNH3PG Approved Insulin-like growth factor 1 receptor (IGF1R) affects the response to substance of Etoposide. [61]
Mitoxantrone DMM39BF Approved Insulin-like growth factor 1 receptor (IGF1R) affects the response to substance of Mitoxantrone. [61]
Afimoxifene DMFORDT Phase 2 Insulin-like growth factor 1 receptor (IGF1R) decreases the response to substance of Afimoxifene. [62]
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This DOT Affected the Regulation of Drug Effects of 1 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Uric acid DMA1MKT Investigative Insulin-like growth factor 1 receptor (IGF1R) affects the abundance of Uric acid. [63]
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10 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Insulin-like growth factor 1 receptor (IGF1R). [2]
Arsenic DMTL2Y1 Approved Arsenic affects the methylation of Insulin-like growth factor 1 receptor (IGF1R). [7]
Fulvestrant DM0YZC6 Approved Fulvestrant increases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [15]
Gefitinib DM15F0X Approved Gefitinib increases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [28]
Insulin-glargine DMR4HIW Approved Insulin-glargine increases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [31]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [40]
BMS-754807 DMPK32V Phase 1 BMS-754807 decreases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [41]
AEW-541 DMQF982 Phase 1 AEW-541 decreases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [42]
BMS 536924 DMDJH2L Preclinical BMS 536924 decreases the phosphorylation of Insulin-like growth factor 1 receptor (IGF1R). [44]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the methylation of Insulin-like growth factor 1 receptor (IGF1R). [45]
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⏷ Show the Full List of 10 Drug(s)
55 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [3]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [4]
Cisplatin DMRHGI9 Approved Cisplatin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [5]
Estradiol DMUNTE3 Approved Estradiol increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [6]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [8]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [9]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [10]
Testosterone DM7HUNW Approved Testosterone increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [10]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [11]
Marinol DM70IK5 Approved Marinol increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [12]
Progesterone DMUY35B Approved Progesterone decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [13]
Menadione DMSJDTY Approved Menadione affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [14]
Dexamethasone DMMWZET Approved Dexamethasone decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [16]
Folic acid DMEMBJC Approved Folic acid decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [17]
Azathioprine DMMZSXQ Approved Azathioprine decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [18]
Ethanol DMDRQZU Approved Ethanol decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [19]
Diclofenac DMPIHLS Approved Diclofenac affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [11]
Menthol DMG2KW7 Approved Menthol decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [20]
Simvastatin DM30SGU Approved Simvastatin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [21]
Gemcitabine DMSE3I7 Approved Gemcitabine decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [22]
Clodronate DM9Y6X7 Approved Clodronate increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [23]
Capsaicin DMGMF6V Approved Capsaicin increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [24]
Enzalutamide DMGL19D Approved Enzalutamide decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [25]
Sorafenib DMS8IFC Approved Sorafenib decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [26]
Hydrocortisone DMGEMB7 Approved Hydrocortisone affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [27]
Methimazole DM25FL8 Approved Methimazole decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [29]
Masoprocol DMMVNZ0 Approved Masoprocol decreases the activity of Insulin-like growth factor 1 receptor (IGF1R). [30]
Tetrahydrofolic acid DMH15UV Approved Tetrahydrofolic acid decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [17]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [30]
Berberine DMC5Q8X Phase 4 Berberine increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [32]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [33]
Epigallocatechin gallate DMCGWBJ Phase 3 Epigallocatechin gallate increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [34]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [26]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [35]
Tocopherol DMBIJZ6 Phase 2 Tocopherol decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [36]
Tanespimycin DMNLQHK Phase 2 Tanespimycin affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [37]
NVP-AUY922 DMTYXQF Phase 2 NVP-AUY922 decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [37]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [39]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [43]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [46]
Formaldehyde DM7Q6M0 Investigative Formaldehyde increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [47]
Milchsaure DM462BT Investigative Milchsaure increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [48]
chloropicrin DMSGBQA Investigative chloropicrin increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [49]
Deguelin DMXT7WG Investigative Deguelin decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [50]
GALLICACID DM6Y3A0 Investigative GALLICACID increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [51]
D-glucose DMMG2TO Investigative D-glucose increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [52]
[3H]methyltrienolone DMTSGOW Investigative [3H]methyltrienolone increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [33]
4-hydroxy-2-nonenal DM2LJFZ Investigative 4-hydroxy-2-nonenal decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [53]
QUERCITRIN DM1DH96 Investigative QUERCITRIN affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [54]
Rapamycin Immunosuppressant Drug DM678IB Investigative Rapamycin Immunosuppressant Drug affects the activity of Insulin-like growth factor 1 receptor (IGF1R). [55]
Aminohippuric acid DMUN54G Investigative Aminohippuric acid affects the expression of Insulin-like growth factor 1 receptor (IGF1R). [56]
Daidzein DMRFTJX Investigative Daidzein decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [35]
Hydroxyestradiol DMJXQME Investigative Hydroxyestradiol increases the expression of Insulin-like growth factor 1 receptor (IGF1R). [57]
Dihydrofolic Acid DM1BDM8 Investigative Dihydrofolic Acid decreases the expression of Insulin-like growth factor 1 receptor (IGF1R). [17]
PQ401 DMVNHTE Investigative PQ401 decreases the activity of Insulin-like growth factor 1 receptor (IGF1R). [58]
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⏷ Show the Full List of 55 Drug(s)
1 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
PIPERINE DMYEAB1 Phase 1/2 PIPERINE affects the binding of Insulin-like growth factor 1 receptor (IGF1R). [38]
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